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br Results and discussion Compounds were tested for
2019-12-03
Results and discussion Compounds were tested for their binding affinity to human CRTH2 in a radioligand binding assay (3H-PGD2) using CHO cells stably transfected with human CRTH2. In addition, these compounds were assessed for their functional activity in PGD2 driven Ca2+ flux in KB8 cells expre
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Since we found that the pharmacokinetic properties of
2019-12-03
Since we found that the pharmacokinetic properties of KPT-185 were unsuitable when given subcutaneously or orally, it is not a candidate for in vivo therapy for NHL. However, the pharmacokinetic properties of KPT-276, a CRM1-inhibiting SINE structurally related to and with functional activities simi
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The importance of AAE in enhancing the
2019-12-03
The importance of AAE3 in enhancing the survival of plants and yeast when confronted with certain environmental stresses has been documented in recent reports. In response to biotic stress such as oxalate-secreting micro-organisms, AAE3 was found to reduce the inhibitory growth effects of the secret
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In an effort to discover additional GPCRs directing the migr
2019-12-03
In an effort to discover additional GPCRs directing the migratory events of responding B cells, we identified Epstein-Barr virus (EBV)-induced gene 2 (EBI2) as a promising candidate. The gene encoding EBI2 (Ebi2, also known as Gpr183) was originally identified together with Ebi1 (Ccr7) as the most h
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VUF 10166 receptor dihydroxycholesterol OHC was recently ide
2019-12-03
7α,25-dihydroxycholesterol (7α,25-OHC) was recently identified by classic analytical methods as a high-affinity ligand for EBI2 (Hannedouche et al., 2011; Liu et al., 2011). 7α,25-OHC was previously identified as an intermediate in the alternate pathway of hepatic bile VUF 10166 receptor synthesis
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br Materials and methods br Results br Discussion Ubiquitina
2019-12-03
Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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Tailoring pharmacological treatment to the
2019-12-03
Tailoring pharmacological treatment to the genetic background of a person can enhance therapeutic response (), increase compliance (), and decrease drug toxicity (, , ). Because cocaine addiction has a strong genetic basis, with the vulnerability to develop an addiction estimated to be as high as 72
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Ligand binding RTK activation induces the
2019-12-03
Ligand binding (RTK activation) induces the endocytic internalization of RTKs, and this has been demonstrated for CSF-1R [15], [16], [17]. Endocytosed RTKs are targeted to the lysosome, which we and others have established to be dependent on ubiquitination via CBL-family and recognition by ESCRT com
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Immune Response and Immune Evasion Up to of the
2019-12-02
Immune Response and Immune Evasion Up to 10% of the host Sodium ascorbate are infected with EBV during acute infectious mononucleosis. Most of these cells are effectively cleared by the immune system, but some downregulate viral gene expression and differentiate into safety in the resting memory B
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br Significance Our understanding of the ubiquitin
2019-12-02
Significance Our understanding of the ubiquitin biology has been rapidly expanding. The role of the ubiquitin system in the pathogenesis of numerous disease states has increased the interest in finding new strategies to pharmacologically interfere with the enzymes responsible of the ubiquitinatio
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As for antiviral activity eight out of synthesized compounds
2019-12-02
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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mpges-1 inhibitors A cocktail approach can detect the
2019-12-02
A cocktail approach can detect the activities of multiple CYP 450 isoforms following administration of multiple CYP-specific substrates in a single experiment. Caffeine, losartan, omeprazole, dextromethorphan and midazolam are often used as substrates in “cocktail probes” of human cytochrome CYP1A2,
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Besides being an energy storing tissue adipose
2019-12-02
Besides being an energy storing tissue, adipose tissue acts as an active endocrine organ that secretes a number of biologically active adipokines involved in multiple physiological processes such as inflammation and lipid and glucose metabolism, with direct and indirect effects on reproduction [15,1
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br Introduction The dopaminergic system and its
2019-12-02
Introduction The dopaminergic system and its projections including both the prefrontal Pioglitazone HCl (PFC) and striatum are known as being crucial to synaptic plasticity, skill acquisition and higher order functions (e.g., working memory and cognitive control; Matsumoto et al., 2003). Variatio
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A widely accepted mechanism to
2019-12-02
A widely accepted mechanism to differentiate hESCs into cardiomyocytes is through perturbation of the canonical Wnt/β-catenin pathway. Initial Wnt activation is required to form the motilin receptor agonist [3]. Thereafter, it is believed that inhibition of the canonical Wnt/β-catenin pathway is pi
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